Icoduline hydrochloride, CBS-113 A-药物合成数据库

【药物名称】Icoduline hydrochloride, CBS-113 A

化学结构式(Chemical Structure):

参考文献No.	5389
标题:	N-Substd. 2-amino-thiazoles, process for their pre
作者:	Alazet, A.; Bonne, C.; Coquelet, C.; Sincholle, D. (Chauvin Laboratories SA)
来源:	EP 0202157; ES 8900045; FR 2581063; JP 1987077375; US 4785008

合成路线图解说明: Condensation of benzoil isothiocyanate (I) with 6-amino-m-cresol in refluxing acetone gives N-benzoyl-N'-(2-hydroxy-4-methylphenyl)thiourea (II), which is hydrolyzed with sodium hydroxide to afford N-(2-hydroxy-4-methyl(phenyl)thiourea (III). Thiazolyl ring closure is obtained by addition of chloroacetaldehyde diethylacetal in refluxing ethanol catalyzed by p-toluenesulfonic acid. 2-(2-Hydroxy-4-methylphenyl)aminothiazole is then converted to its hydrochloride sait by bubbling gaseous hydrochloric acid.

参考文献No.	56412
标题:	CBS-113 A
作者:	Coquelet, C.; Bonne, C.
来源:	Drugs Fut 1987,12(6),525

合成路线图解说明: Condensation of benzoil isothiocyanate (I) with 6-amino-m-cresol in refluxing acetone gives N-benzoyl-N'-(2-hydroxy-4-methylphenyl)thiourea (II), which is hydrolyzed with sodium hydroxide to afford N-(2-hydroxy-4-methyl(phenyl)thiourea (III). Thiazolyl ring closure is obtained by addition of chloroacetaldehyde diethylacetal in refluxing ethanol catalyzed by p-toluenesulfonic acid. 2-(2-Hydroxy-4-methylphenyl)aminothiazole is then converted to its hydrochloride sait by bubbling gaseous hydrochloric acid.